Abstract

Purpose of the study: The antiretroviral therapy (ART) has dramatically improved human immunodefi ciency virus (HIV)/ acquired immunodefi ciency syndrome (AIDS) treatment, prevention and also has been found to increase the lifespan
of HIV/AIDS patients by providing durable control of the HIV replication in patients. Efavirenz is a non-nucleoside
reverse transcriptase inhibitor of HIV-1. The purpose of this study is to formulate efavirenz-loaded bovine serum
albumin nanoparticles to improve efavirenz delivery into various organs. Materials and Methods: Nanoparticles were
prepared by desolvation technique and coated with polysorbate 80. Ethanol, glutaraldehyde, and mannitol were used
as desolvating, cross linking agent, and cryoprotectant, respectively. Drug to polymer ratio was chosen at fi ve levels
from 1:2, 1:3, 1:4, 1:5, and 1:6 (by weight). The formulated nanoparticles were characterized for Fourier Transform
Infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC) studies, entrapment effi ciency, particle size,
surface charge, surface morphology, in vitro drug release, release kinetics, stability studies, and biodistribution studies.
Results and Major Conclusion: The particle size of the prepared formulations was found below 250nm with narrow
size distribution, spherical in shape and showed good entrapment effi ciency (45.62–72.49%). The in vitro drug release
indicated biphasic release and its data were fi tted to release kinetics models and release pattern was Fickian diffusion
controlled release profi le. The prepared nanoparticles increased efavirenz delivery into various organs by several fold in
comparison with the free drug.